2-AMINOALKYL-5-AMINOALKYLAMINO SUBSTITUTED ISOQUINOINDAZOL-6-(2H)ONES, PROCESS FOR PREPARING THEREOF, PHARMCOMPOSITION AND METHOD OF TREATMENT OF TUMOR

FIELD: pharmacology and medicine. SUBSTANCE: R is hydrogen or hydroxy; one of X and Y is carbon atom and the other is nitrogen atom provided that when Y is nitrogen and R is hydrogen; A and B are the same or different and are selected from the group C-Calkyl or phenylalkyl; C-Calkyl having one or tw...

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Hauptverfasser: A.POL KRAPCHO, EHRNESTO MENTA, AMBRODZHIO OLIVA, SIL'VANO SPINELLI
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: pharmacology and medicine. SUBSTANCE: R is hydrogen or hydroxy; one of X and Y is carbon atom and the other is nitrogen atom provided that when Y is nitrogen and R is hydrogen; A and B are the same or different and are selected from the group C-Calkyl or phenylalkyl; C-Calkyl having one or two substituents selected from the group consisting of ORand NRR; C-Calkyl interrupted by one or two oxygen atoms or -MRgroup; said C-Calkyl is optionally substituted by one or two hydroxy (OH) or NRRgroups; Ris selected from the group consisting of hydrogen, C-Calkyl, phenyl, phenylalkyl, S(O)R, C-Calkyl optionally substituted by NRR;; Rand Rare the same or different and are selected from the group consisting of hydrogen, C-Calkyl, phenylalkylphenyl, C-Calkyl substituted by one or two hydroxy (OH) groups, or Rand Rtogether with nitrogen atom they are attached form ethyleneimine ring or 5- or 6-member aromatic or unaromatic heterocyclic ring optionally containing other heteroatoms such as sulfur, oxygen or nitrogen, Ris selected from the group consisting of hydrogen C-Calkyl, C-Chydroxyalkyl, C-Calkyl substituted NRRRphenylalkyl, phenyl; C-Cis selected from the group consisting ofalkyl or phenylalkyl as free bases and salts thereof with pharmaceutically acceptable acids. These compounds show antitumor activity. EFFECT: improved properties of the pharmcomposition and more efficient method of treating tumor. Соединения общей формулы, данной в описании, в виде свободных оснований и их солей с фармацевтически приемлемыми кислотами. Эти соединения показывают антиопухолевую активность.